Anti HIV-1 Agents 6. Synthesis and Anti-HIV-1 Activity of Indolyl Glyoxamides

Title:Anti HIV-1 Agents 6. Synthesis and Anti-HIV-1 Activity of Indolyl Glyoxamides

Volume: 8 Issue: 5

Author(s): Yi Wang, Ning Huang, Xiang Yu, Liu-Meng Yang, Xiao-Yan Zhi, Yong-Tang Zheng and Hui Xu

Affiliation:

Keywords: Indolyl glyoxamide, Acquired immunodeficiency syndrome, Human immunodeficiency virus-1, Inhibitor, antifungal, atom, HIV, AIDS, oxalyl chloride, NMR

Abstract: In order to discover compounds with superior anti-human immunodeficiency virus type 1 (HIV-1) activity, 9 new indolyl glyoxamide derivatives (3a-i) were synthesized and preliminarily evaluated as HIV-1 inhibitors in vitro. Among all the derivatives, especially compounds 3e and 3h showed the potent anti-HIV-1 activity with EC50 values of 6.83 and 4.35 μg/mL, and TI values of >27.15 and 49.45, respectively. It demonstrated that introduction of the substituent R3 as the halogen atom and the position of R3 were generally important to their activity.

Cite this article as:

Wang Yi, Huang Ning, Yu Xiang, Yang Liu-Meng, Zhi Xiao-Yan, Zheng Yong-Tang and Xu Hui, Anti HIV-1 Agents 6. Synthesis and Anti-HIV-1 Activity of Indolyl Glyoxamides, Medicinal Chemistry 2012; 8 (5) . https://dx.doi.org/10.2174/157340612802084270